Substituted tetracyclic oxazepine and thiazepine derivatives with 5-HT2 receptor affinity

摘要

PCT No. PCT/EP95/04197 Sec. 371 Date Apr. 25, 1997 Sec. 102(e) Date Apr. 25, 1997 PCT Filed Oct. 25, 1995 PCT Pub. No. WO96/14321 PCT Pub. Date May 17, 1996This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. IMAGE (I) wherein: R1 and R2 each independently are hydrogen; C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 to R10 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; R11 is hydrogen, C1-6alkyl, or trifluoromethyl; R12 is hydrogen, C1-6alkyl, cyano, or trifluoromethyl; n is zero to 6; and X is O, S, S(=O) or S(=O)2. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.